In vitro studies have suggested that the glutathione (GSH) S-transferase (GST)-catalyzed GSH conjugation is an important mechanism for the detoxification of (+)-anti-7,8-dihydroxy-9,10-epoxy-7,8,9,10-tetrahydrobenzo[a]pyrene [(+)-anti-BPDE], which is the activated form of the widespread environm...
The role of glutathione (GSH) and total non-protein thiols (NPSH) in repairing radiation-induced free radical damage incurred under aerated and hypoxic conditions was investigated using Chinese hamster V79 cells cultured in vitro. GSH and NPSH levels were depleted in V79 cells of varying cell de...
Buthionine sulphoximine (BSO) selectively inhibits glutathione (GSH) synthesis and may enhance the antineuroblastoma activity of melphalan (L-PAM). We determined the cytotoxicity of BSO (dose range 0–1000 μM) alone and in combination with L-PAM (dose range 0–0 μM) in a panel of 18 human neur...
l-buthionine-S,R-sulfoximine (l-S,R-BSO) was enriched for the active l-buthionine-S-sulfoximine (l-S-BSO) diastereomer. Comparative analysis was performed to determine if this enriched form possessed an increased capacity to deplete glutathione (GSH), and to inhibit the proliferation of tumor ce...
Glutathione (GSH) depletion is widely used to sensitize cells to anticancer treatment inducing the progression of programmed cell death and overcoming chemoresistance. It has been reported that neuroblastoma cells with MYCN amplification are unable to start TRAIL-dependent death and MYCN, in con...
l-Buthionine sulfoximine (BSO) is a potent inhibitor of glutathione biosynthesis and studies have shown that it is capable of enhancing the apoptotic effects of several chemotherapeutic agents. Previous studies have shown that long-term antihormonal therapy leads to acquired drug resistance and ...
Glutathione is the major antioxidant in the living cells. Its deficit has been linked to neurodegenerative disorders as Parkinson's disease but its role in the etiology of nigral degeneration and sensory-motor performance has been poorly explored. To evaluate the effect of glutathione deple...
l-S,R-buthionine sulfoximine (l-S,R BSO) is a potent specific inhibitor of γ-glutamylcysteine synthetase, the rate-limiting step in glutathione (GSH) biosynthesis. GSH is an important component of tumor drug resistance based on a strong association and recent transfection studies. Depletion of ...
Purpose: To develop dosing criteria for the use of L-buthionine-S-sulfoximine (active diastereoisomer) as a glutathione depletor in the clinic, using a pharmacodynamic and pharmacokinetic in vitro-in vivo approach.Methods and Materials: In vitro: L-buthionine-S-sulfoximine uptake was determined ...
Glutathione (GSH) and ascorbate, the cytoplasmic antioxidants, can regenerate and replace each other in scavenging reactive oxygen species reaction. Mice, but not guinea pigs, produce ascorbate endogenously. l-Buthionine-S,R-sulfoximine (L-S,R-BSO) substantially inhibited GSH production at a gre...
Glutathione (GSH) is an essential component of intracellular antioxidant systems that plays a primordial role in the protection of cells against oxidative stress, maintaining redox homeostasis and xenobiotic detoxification. GSH synthesis in the brain is limited by the availability of cysteine an...
The aims of the present work were to evaluate the exploratory activity in Sprague-Dawley rats, as well as to analyze the nigral and striatal mRNA expression of the plasticity-related genes bdnf and arc after L-buthionine sulfoximine (BSO) injection into substantia nigra compacta. Lesioned rats t...
Mo-CBP3 is a chitin-binding 2S albumin from Moringa oleifera. This seed storage protein is resistant to thermal denaturation and shows biological activities that might be of practical use, such as antifungal properties against Candida sp., a pathogen that causes candidiasis, and against Fusarium...
This study aimed to develop non-food fermentation for the cost-effective production of poly-(γ-glutamic acid) (γ-PGA) using a novel strain of Bacillus amyloliquefaciens NX-2S. The new isolate assimilated inulin more efficiently than other carbohydrates from Jerusalem artichoke, without hydroly...
Non-toxic cultured juvenile kusafugu Fugu niphobles were fed with a diet containing highly toxic natural komonfugu Fugu poecilonotus liver until the 30th day (8.0 μg of TTX and 3.7 μg of 4,9-anhydroTTX/fish/day), and then fed with a non-toxic diet until the 240th day. During the 30–240th day,...
The voltage-gated sodium ion channel inhibitory activities of four tetrodotoxin analogues were evaluated for their ability to reduce the cytotoxicity of ouabain and veratridine in mouse neuroblastoma Neuro-2a cells. EC50 of the novel analogue, 4,4a-anhydrotetrodotoxin purified from pufferfish, w...
The actions of the newly discovered 4-epitetrodotoxin and of anhydrotetrodotoxin have been studied on the internally perfused squid giant axon under voltage-clamped conditions. Both compounds are selective in blocking only the sodium channel. The concentration for reducing the sodium current to ...
7-Oxo-7-deacetoxygedunin, a limonoid isolated fromGuarea grandiflora(Meliaceae) has been found to act as an inhibitor of photophosphorylation in spinach thylakoids. ATP synthesis and phosphorylating electron flows were inhibited by 88 and 83%, respectively, at 300 μM of 7-oxo-7-deacetoxygedunin...
Osteoclasts together with osteoblasts play pivotal roles in bone remodeling. Aberrations in osteoclast differentiation and activity contribute to osteopenic disease. Osteoclasts differentiate from monocyte/macrophage progenitors, a process that is initiated by the interaction between receptor ac...
A new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1). Our initial compound 5a showed a weak inhibitory activity. Significant improvements in potency were achieved by substituent...
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